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Enzymes for Research, Diagnostic and Industrial Use

BM-1074

Cat No.
CEI-0874
Description
BM-1074 is a potent and efficacious Bcl-2/Bcl-xL inhibitor with Ki of <1 nM, inactive to Mcl-1.
CAS No.
1391108-10-3
Molecular Weight
1013.68
Storage
2 years -20 centigrade Powder; 2 weeks 4 centigrade in DMSO; 6 months -80 centigrade in DMSO.
Targets
Bcl-2/Bcl-xL
IC50
1 nM (Ki)
Molecular Formula
C50H57ClN8O7S3
Chemical Name
1H-Pyrrole-3-carboxamide, 5-(4-chlorophenyl)-4-[3-[4-[4-[[[4-[[(1R)-3-(dimethylamino)-1-[(phenylthio)methyl]propyl]amino]-3-nitrophenyl]sulfonyl]amino]phenyl]-1-piperazinyl]phenyl]-2-methyl-1-(1-methylethyl)-N-(methylsulfonyl)-
Solubility
DMSO mg/mL; Water mg/mL; Ethanol mg/mL
In vitro
BM-1074 inhibits FP-based binding affinities of Bcl-2/Bcl-xL with IC50 of 1.8 and 6.9 nM, respectively. BM-1074 inhibits growth of small-cell lung cancer cell lines H1963, H187 and H1417 with IC50 of 1, 1.4 and 2.3 nM.
In vivo
BM-1074, administrated at a single dose of 15 mg/kg, induces robust cleavage of PARP and caspase-3 at both 3 and 6 h time points in H146 xenograft tumor tissues. BM-1074 (15 mg/kg) is capable of achieving rapid, complete, and persistent tumor regression. 18 days after the treatment is ended, none of the mice treated with BM-1074 has measurable tumors, and 74 days after the end of the treatment with BM-1074, 50 % animals do not have measurable tumors. The average tumor size for the all mice are 47 mm3 at day 117, as compared to 130 mm3 at the start of the treatment. All the mice treated with compound BM-1074 suffers no significant weight loss (<5%) and do not show other signs of toxicity during or after the treatment.
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